Medicinal Chemistry Research p. 503 - 517 (2014)
Update date:2022-08-02
Topics:
Dhakane, Valmik D.
Chavan, Hemant V.
Thakare, Vishnu N.
Adsul, Laxman K.
Shringare, Sadanand N.
Bandgar, Babasaheb P.
In the present study, we evaluated the anti-inflammatory activity with pharmacokinetic, ulcerogenic properties of various synthesized prodrugs of ibuprofen in experimental animals. Prodrugs 2, 6, 9, 10, 12, and 14 were found to possess significant anti-inflammatory activity with almost non-ulcerogenic potential than standard drug ibuprofen 1a in both normal and inflammation-induced rats. Metabolic stability of prodrugs 2, 6, 9, 10, 12, and 14 were also studied in rat liver microsomes and oral bioavailability was determined by estimating area under curve (AUC) and plasma concentration of these prodrugs at various time intervals. The experimental findings elicited higher AUC and plasma concentration at 1 and 2 h indicating improved oral bioavailability as compared to parent ibuprofen. These prodrugs are found to have least gastric ulceration with retain anti-inflammatory activity observed in experimental animals. Therefore, present experimental findings demonstrated significant improvement of various pharmacokinetic properties with least ulcerogenic potential of ester prodrugs of ibuprofen an anti-inflammatory agent
View MoreTianjin Hedong Red Cliff Chemical Reagent Factory
Contact:+86-022-84780548
Address:Li Ming Zhuang Gong Ye Yuan,Dongli District,Tianjin,China
Shanghai Run-Biotech Co., Ltd.
website:http://www.run-biotech.com
Contact:+86-21-31576854/57171705 / 57171706
Address:second floor, building 3, No.999, jiangyue Road, minghang District, Shanghai, China
Henan zhongda Biological Engineering Co., Ltd
Contact:86-28-18109029985
Address:shenzhou road,xuedian industrial estate,zhengzhou city,henan province CHN
Shandong General Materials Co.,Ltd(Shandong Aoertong Chemical Co., Ltd)
Contact:86-531-88072280
Address:No. 1825 Hualong Road, Licheng District, Jinan, Shandong, China
Xi'an North Information Industry Co., Ltd. Weilv Chemical Department
Contact:+86-29-88156413
Address:Jixiang Road 99 Xi'an Shaanxi Province
Doi:10.1055/s-0030-1259519
(2011)Doi:10.1016/j.bmc.2017.02.029
(2017)Doi:10.1016/j.tetlet.2010.10.076
(2011)Doi:10.1021/ja00180a033
(1990)Doi:10.1016/j.bmc.2010.12.017
(2011)Doi:10.1039/j29660000750
(1966)